HK1046681B - 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use - Google Patents

6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use

Info

Publication number
HK1046681B
HK1046681B HK02108204.3A HK02108204A HK1046681B HK 1046681 B HK1046681 B HK 1046681B HK 02108204 A HK02108204 A HK 02108204A HK 1046681 B HK1046681 B HK 1046681B
Authority
HK
Hong Kong
Prior art keywords
alkinyl
alkenyl
epoxy
production
epothilone derivatives
Prior art date
Application number
HK02108204.3A
Other languages
Chinese (zh)
Other versions
HK1046681A1 (en
Inventor
烏爾里希‧克拉爾
沃爾夫岡‧施韋德
維爾納‧什庫巴拉
貝恩德‧比希曼
延斯‧霍夫曼
羅斯瑪麗‧利希特納
Original Assignee
舍林股份公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE19921086A external-priority patent/DE19921086A1/en
Priority claimed from DE19954228A external-priority patent/DE19954228A1/en
Priority claimed from DE10015836A external-priority patent/DE10015836A1/en
Application filed by 舍林股份公司 filed Critical 舍林股份公司
Publication of HK1046681A1 publication Critical patent/HK1046681A1/en
Publication of HK1046681B publication Critical patent/HK1046681B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
HK02108204.3A 1999-04-30 2002-11-13 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use HK1046681B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE19921086A DE19921086A1 (en) 1999-04-30 1999-04-30 New stable 6-alkenyl- or 6-alkynyl-epothilone derivatives, are cell division regulators useful for treating malignant tumors, angiogenesis or chronic inflammatory disease
DE19954228A DE19954228A1 (en) 1999-11-04 1999-11-04 New epothilone derivatives used for treating e.g. malignant melanoma, breast carcinoma, psoriasis, multiple sclerosis and arthritis
DE10015836A DE10015836A1 (en) 2000-03-27 2000-03-27 New epothilone derivatives used for treating e.g. malignant melanoma, breast carcinoma, psoriasis, multiple sclerosis and arthritis
PCT/IB2000/000657 WO2000066589A1 (en) 1999-04-30 2000-05-01 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations

Publications (2)

Publication Number Publication Date
HK1046681A1 HK1046681A1 (en) 2003-01-24
HK1046681B true HK1046681B (en) 2008-08-29

Family

ID=27213767

Family Applications (1)

Application Number Title Priority Date Filing Date
HK02108204.3A HK1046681B (en) 1999-04-30 2002-11-13 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use

Country Status (33)

Country Link
EP (1) EP1173441B1 (en)
JP (2) JP4024003B2 (en)
KR (1) KR100721488B1 (en)
CN (1) CN100368415C (en)
AR (1) AR023792A1 (en)
AT (1) ATE440847T1 (en)
BG (1) BG65601B1 (en)
BR (1) BR0010190A (en)
CA (2) CA2371226C (en)
CY (1) CY1109768T1 (en)
CZ (1) CZ299653B6 (en)
DE (1) DE60042821D1 (en)
DK (1) DK1173441T3 (en)
EA (1) EA011502B1 (en)
EE (1) EE05292B1 (en)
ES (1) ES2331506T3 (en)
HK (1) HK1046681B (en)
HR (1) HRP20010892A2 (en)
HU (1) HUP0201010A3 (en)
IL (1) IL145938A0 (en)
ME (1) MEP13908A (en)
MX (1) MXPA01011039A (en)
NO (1) NO328149B1 (en)
NZ (1) NZ514989A (en)
PE (1) PE20010116A1 (en)
PL (1) PL210762B1 (en)
PT (1) PT1173441E (en)
RS (1) RS51023B (en)
SI (1) SI1173441T1 (en)
SK (1) SK286858B6 (en)
TW (2) TWI294292B (en)
WO (1) WO2000066589A1 (en)
ZA (1) ZA200109859B (en)

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EP1367057B1 (en) 1996-11-18 2008-09-17 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilones E and F
AU756699B2 (en) 1996-12-03 2003-01-23 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
US6365749B1 (en) 1997-12-04 2002-04-02 Bristol-Myers Squibb Company Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
US6498257B1 (en) 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
US6399638B1 (en) 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified epothilone derivatives
US6518421B1 (en) * 2000-03-20 2003-02-11 Bristol-Myers Squibb Company Process for the preparation of epothilone analogs
US6593115B2 (en) 2000-03-24 2003-07-15 Bristol-Myers Squibb Co. Preparation of epothilone intermediates
DE10020899A1 (en) * 2000-04-20 2001-10-25 Schering Ag New 9-oxa-epothilone derivatives, are phase-specific cell division regulators useful for treating malignant tumors, angiogenesis or inflammatory disease
UA75365C2 (en) 2000-08-16 2006-04-17 Bristol Myers Squibb Co Epothilone analog polymorph modifications, a method for obtaining thereof (variants), a pharmaceutical composition based thereon
MXPA03006485A (en) 2001-01-25 2003-09-22 Bristol Myers Squibb Co Parenteral formulation containing epothilone analogs.
NZ526871A (en) * 2001-01-25 2006-01-27 Bristol Myers Squibb Co Pharmaceutical dosage forms of epothilones for oral administration
CZ20032021A3 (en) 2001-01-25 2004-05-12 Bristol@Myersásquibbácompany Methods for administering epothilone analogs when treating cancer ration methods
HUP0303175A2 (en) 2001-02-20 2003-12-29 Bristol-Myers Squibb Co. Use of epothlone derivatives for preparation of pharmaceutical composition suitable for treatment of refractory tumors
IL157128A0 (en) 2001-02-20 2004-02-08 Bristol Myers Squibb Co Pharmaceutical compositions containing epothilone derivatives
JP2004529904A (en) 2001-03-14 2004-09-30 ブリストル−マイヤーズ スクイブ カンパニー Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
CA2449077A1 (en) 2001-06-01 2002-12-12 Gregory D. Vite Epothilone derivatives
EP1340498A1 (en) * 2002-03-01 2003-09-03 Schering Aktiengesellschaft Use of epothilones in the treatment of brain diseases associated with proliferative processes
DE60330651D1 (en) 2002-03-12 2010-02-04 Bristol Myers Squibb Co C3-cyanoepothilonderivate
US7211593B2 (en) 2002-03-12 2007-05-01 Bristol-Myers Squibb Co. C12-cyano epothilone derivatives
TW200403994A (en) 2002-04-04 2004-03-16 Bristol Myers Squibb Co Oral administration of EPOTHILONES
TW200400191A (en) 2002-05-15 2004-01-01 Bristol Myers Squibb Co Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
AU2003243561A1 (en) 2002-06-14 2003-12-31 Bristol-Myers Squibb Company Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
ES2439995T3 (en) 2002-09-23 2014-01-27 Bristol-Myers Squibb Company Preparation, isolation and purification procedures for epothilone B
DE10361794B3 (en) * 2003-12-31 2005-10-06 Schering Ag Optically active heteroaromatic β-hydroxy esters and processes for their preparation and their use as intermediates in the epothilone total synthesis
EP1559447A1 (en) 2004-01-30 2005-08-03 Institut National De La Sante Et De La Recherche Medicale (Inserm) Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism
EP1640004A1 (en) * 2004-09-24 2006-03-29 Schering Aktiengesellschaft Use of epothilones in the treatment of bone metastases and bone tumors or cancers
US20060121511A1 (en) 2004-11-30 2006-06-08 Hyerim Lee Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents
EP1674098A1 (en) 2004-12-23 2006-06-28 Schering Aktiengesellschaft Stable and tolerable parental formulations of highly reactive organic drug substances with low or no solubility in water
CN100384419C (en) * 2005-12-02 2008-04-30 菏泽睿鹰制药集团有限公司 Epothilone slow-release implanting composition and use
DE102007016046A1 (en) 2007-03-30 2008-10-23 Bayer Schering Pharma Aktiengesellschaft Process for the preparation of epothilone derivatives by selective catalytic epoxidation
EP2065054A1 (en) 2007-11-29 2009-06-03 Bayer Schering Pharma Aktiengesellschaft Combinations comprising a prostaglandin and uses thereof
EP2070521A1 (en) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Surface-modified nanoparticles
DE102007059752A1 (en) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Functionalized solid polymer nanoparticles containing epothilones
EP2210584A1 (en) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Stable polymeric composition comprising an epothilone and an amphiphilic block copolymer
EP3566719A1 (en) 2010-05-18 2019-11-13 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases
CA2858806A1 (en) 2011-12-23 2013-06-27 Innate Pharma Enzymatic conjugation of polypeptides
EP2872894B1 (en) 2012-07-13 2019-04-17 Innate Pharma Screening of conjugated antibodies
WO2014072482A1 (en) 2012-11-09 2014-05-15 Innate Pharma Recognition tags for tgase-mediated conjugation
WO2014140300A1 (en) 2013-03-15 2014-09-18 Innate Pharma Solid phase tgase-mediated conjugation of antibodies
EP3010547B1 (en) 2013-06-20 2021-04-21 Innate Pharma Enzymatic conjugation of polypeptides
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IL134419A0 (en) * 1997-08-09 2001-04-30 Schering Ag Epothilone derivatives, process for the preparation thereof and pharmaceutical compositions containing the same

Also Published As

Publication number Publication date
WO2000066589A1 (en) 2000-11-09
IL145938A0 (en) 2002-07-25
PE20010116A1 (en) 2001-02-15
SK15512001A3 (en) 2002-05-09
HRP20010892A2 (en) 2008-06-30
CN1349534A (en) 2002-05-15
JP4886578B2 (en) 2012-02-29
CZ299653B6 (en) 2008-10-08
CN100368415C (en) 2008-02-13
HK1046681A1 (en) 2003-01-24
TWI294292B (en) 2008-03-11
TW200711679A (en) 2007-04-01
CA2651653C (en) 2012-02-14
DK1173441T3 (en) 2009-12-07
NZ514989A (en) 2004-02-27
ZA200109859B (en) 2003-02-28
CA2371226A1 (en) 2000-11-09
EE200100568A (en) 2003-02-17
JP2007224038A (en) 2007-09-06
PT1173441E (en) 2009-11-06
MEP13908A (en) 2010-06-10
MXPA01011039A (en) 2003-06-30
CA2371226C (en) 2011-11-29
EE05292B1 (en) 2010-04-15
EA011502B1 (en) 2009-04-28
CZ20013885A3 (en) 2002-04-17
EP1173441B1 (en) 2009-08-26
JP4024003B2 (en) 2007-12-19
SI1173441T1 (en) 2010-01-29
NO20015278L (en) 2001-12-21
EP1173441A1 (en) 2002-01-23
ATE440847T1 (en) 2009-09-15
CA2651653A1 (en) 2000-11-09
DE60042821D1 (en) 2009-10-08
PL210762B1 (en) 2012-02-29
NO20015278D0 (en) 2001-10-29
ES2331506T3 (en) 2010-01-07
EA200101025A1 (en) 2002-06-27
HUP0201010A2 (en) 2002-08-28
NO328149B1 (en) 2009-12-21
PL351491A1 (en) 2003-04-22
SK286858B6 (en) 2009-06-05
BG65601B1 (en) 2009-02-27
BG106053A (en) 2002-05-31
AR023792A1 (en) 2002-09-04
TWI280962B (en) 2007-05-11
JP2002543203A (en) 2002-12-17
CY1109768T1 (en) 2014-09-10
RS51023B (en) 2010-10-31
HUP0201010A3 (en) 2005-02-28
KR20020005737A (en) 2002-01-17
KR100721488B1 (en) 2007-05-23
YU77601A (en) 2005-07-19
BR0010190A (en) 2002-01-08

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PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20130501